Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes

Autores
Prieto, Maria Jimena; Temprana, Carlos Facundo; del Río Zabala, Nahuel Eduardo; Marotta, Cristian Hernán; Alonso, Silvia del Valle
Año de publicación
2011
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%). As new strategies to improve treatments efficiency are needed, we have studied cationic G4 PAMAM dendrimers’ performance to act as efficient nanocarriers for this therapeutic drug. In this respect, we explored dendrimererisperidone complexation dependence on solvent, temperature, pH and salt concentration, as well as in vitro cytotoxicity measured on L929 cell line and human red blood cells. The best dendrimererisperidone incorporation was achieved when a mixture of 70:30 and 90:10 v/v chloroform:methanol was used, obtaining 17 and 32 risperidone molecules per dendrimer, respectively. No cytotoxicity on L929 cells was found when dendrimer concentration was below 3 x 10 -2 µM and risperidone concentration below 5.1 µM. Also, no significant hemolysis or morphological changes were observed on human red blood cells. Finally, attempting to obtain an efficient drug delivery system for risperidone, incorporation in G4 PAMAM dendrimers was optimized, improving drug solubility with low cytotoxicity.
Fil: Prieto, Maria Jimena. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Temprana, Carlos Facundo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
Fil: del Río Zabala, Nahuel Eduardo. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
Fil: Marotta, Cristian Hernán. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
Fil: Alonso, Silvia del Valle. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
Materia
Poly(amidoamine) dendrimers
PAMAM G4
Risperidone
Cytotoxicity
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/102455
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/102455
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexesPrieto, Maria JimenaTemprana, Carlos Facundodel Río Zabala, Nahuel EduardoMarotta, Cristian HernánAlonso, Silvia del VallePoly(amidoamine) dendrimersPAMAM G4RisperidoneCytotoxicityhttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%). As new strategies to improve treatments efficiency are needed, we have studied cationic G4 PAMAM dendrimers’ performance to act as efficient nanocarriers for this therapeutic drug. In this respect, we explored dendrimererisperidone complexation dependence on solvent, temperature, pH and salt concentration, as well as in vitro cytotoxicity measured on L929 cell line and human red blood cells. The best dendrimererisperidone incorporation was achieved when a mixture of 70:30 and 90:10 v/v chloroform:methanol was used, obtaining 17 and 32 risperidone molecules per dendrimer, respectively. No cytotoxicity on L929 cells was found when dendrimer concentration was below 3 x 10 -2 µM and risperidone concentration below 5.1 µM. Also, no significant hemolysis or morphological changes were observed on human red blood cells. Finally, attempting to obtain an efficient drug delivery system for risperidone, incorporation in G4 PAMAM dendrimers was optimized, improving drug solubility with low cytotoxicity.Fil: Prieto, Maria Jimena. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Temprana, Carlos Facundo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; ArgentinaFil: del Río Zabala, Nahuel Eduardo. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; ArgentinaFil: Marotta, Cristian Hernán. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; ArgentinaFil: Alonso, Silvia del Valle. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; ArgentinaElsevier France-editions Scientifiques Medicales Elsevier2011-03info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/102455Prieto, Maria Jimena; Temprana, Carlos Facundo; del Río Zabala, Nahuel Eduardo; Marotta, Cristian Hernán; Alonso, Silvia del Valle; Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes; Elsevier France-editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 46; 3; 3-2011; 845-8500223-5234CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0223523410008779info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejmech.2010.12.021info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-11-12T09:59:55Zoai:ri.conicet.gov.ar:11336/102455instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-11-12 09:59:56.064CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
title Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
spellingShingle Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
Prieto, Maria Jimena
Poly(amidoamine) dendrimers
PAMAM G4
Risperidone
Cytotoxicity
title_short Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
title_full Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
title_fullStr Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
title_full_unstemmed Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
title_sort Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes
dc.creator.none.fl_str_mv Prieto, Maria Jimena
Temprana, Carlos Facundo
del Río Zabala, Nahuel Eduardo
Marotta, Cristian Hernán
Alonso, Silvia del Valle
author Prieto, Maria Jimena
author_facet Prieto, Maria Jimena
Temprana, Carlos Facundo
del Río Zabala, Nahuel Eduardo
Marotta, Cristian Hernán
Alonso, Silvia del Valle
author_role author
author2 Temprana, Carlos Facundo
del Río Zabala, Nahuel Eduardo
Marotta, Cristian Hernán
Alonso, Silvia del Valle
author2_role author
author
author
author
dc.subject.none.fl_str_mv Poly(amidoamine) dendrimers
PAMAM G4
Risperidone
Cytotoxicity
topic Poly(amidoamine) dendrimers
PAMAM G4
Risperidone
Cytotoxicity
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%). As new strategies to improve treatments efficiency are needed, we have studied cationic G4 PAMAM dendrimers’ performance to act as efficient nanocarriers for this therapeutic drug. In this respect, we explored dendrimererisperidone complexation dependence on solvent, temperature, pH and salt concentration, as well as in vitro cytotoxicity measured on L929 cell line and human red blood cells. The best dendrimererisperidone incorporation was achieved when a mixture of 70:30 and 90:10 v/v chloroform:methanol was used, obtaining 17 and 32 risperidone molecules per dendrimer, respectively. No cytotoxicity on L929 cells was found when dendrimer concentration was below 3 x 10 -2 µM and risperidone concentration below 5.1 µM. Also, no significant hemolysis or morphological changes were observed on human red blood cells. Finally, attempting to obtain an efficient drug delivery system for risperidone, incorporation in G4 PAMAM dendrimers was optimized, improving drug solubility with low cytotoxicity.
Fil: Prieto, Maria Jimena. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Temprana, Carlos Facundo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
Fil: del Río Zabala, Nahuel Eduardo. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
Fil: Marotta, Cristian Hernán. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
Fil: Alonso, Silvia del Valle. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Biomembranas; Argentina
description Risperidone is an approved antipsychotic drug belonging to the chemical class of benzisoxazole. This drug has low solubility in aqueous medium and poor bioavailability due to extensive first-pass metabolism and high protein binding (>90%). As new strategies to improve treatments efficiency are needed, we have studied cationic G4 PAMAM dendrimers’ performance to act as efficient nanocarriers for this therapeutic drug. In this respect, we explored dendrimererisperidone complexation dependence on solvent, temperature, pH and salt concentration, as well as in vitro cytotoxicity measured on L929 cell line and human red blood cells. The best dendrimererisperidone incorporation was achieved when a mixture of 70:30 and 90:10 v/v chloroform:methanol was used, obtaining 17 and 32 risperidone molecules per dendrimer, respectively. No cytotoxicity on L929 cells was found when dendrimer concentration was below 3 x 10 -2 µM and risperidone concentration below 5.1 µM. Also, no significant hemolysis or morphological changes were observed on human red blood cells. Finally, attempting to obtain an efficient drug delivery system for risperidone, incorporation in G4 PAMAM dendrimers was optimized, improving drug solubility with low cytotoxicity.
publishDate 2011
dc.date.none.fl_str_mv 2011-03
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/102455
Prieto, Maria Jimena; Temprana, Carlos Facundo; del Río Zabala, Nahuel Eduardo; Marotta, Cristian Hernán; Alonso, Silvia del Valle; Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes; Elsevier France-editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 46; 3; 3-2011; 845-850
0223-5234
CONICET Digital
CONICET
url http://hdl.handle.net/11336/102455
identifier_str_mv Prieto, Maria Jimena; Temprana, Carlos Facundo; del Río Zabala, Nahuel Eduardo; Marotta, Cristian Hernán; Alonso, Silvia del Valle; Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer–risperidone complexes; Elsevier France-editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 46; 3; 3-2011; 845-850
0223-5234
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0223523410008779
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejmech.2010.12.021
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier France-editions Scientifiques Medicales Elsevier
publisher.none.fl_str_mv Elsevier France-editions Scientifiques Medicales Elsevier
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 12.976206

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